Intra-Cellular Therapies, Inc. (ITI) announced at a recent conference on neuropsychiatric diseases the results from a recently completed Phase I clinical study demonstrating ITI-007, the Company's lead antipsychotic drug, interacts with important targets in the living human brain. These key targets are critical to drug action in many neuropsychiatric and related disorders. Using positron emission tomography (PET) to image receptor interactions, ITI-007 produced dose-related and long-lasting occupancy of three key targets of psychotropic drug action: the serotonin 5-HT2A and dopamine D2 receptors, as well as the serotonin reuptake transporter (SERT). At low doses, ITI-007 selectively occupies 5-HT2A receptors in the brains of normal healthy volunteers. At a dose of 10 mg, neocortical 5-HT2A receptors are fully occupied and the first evidence is seen of D2 receptor occupancy in the basal ganglia. This 10 mg dose has been shown previously to be particularly effective in improving sleep in patients with sleep maintenance problems.
As the dose of ITI-007 is increased, dose-dependent and progressively increasing amounts of D2 occupancy are achieved, reaching 40% peak occupancy in the basal ganglia at the 40 mg dose (the highest dose tested in this study). At this dose, ITI-007 also demonstrates significant occupancy of the SERT. Moreover, when these targets are occupied in the presence of fully saturated 5-HT2A receptors, effects should be amplified.
"We are pleased to have demonstrated ITI-007's potent interactions with key brain targets in humans," stated Sharon Mates, Chief Executive Officer of Intra-Cellular Therapies. "The simultaneous occupancy of these targeted receptors is unprecedented for antipsychotic drugs. We believe that these results will translate into a reduced need to impose high doses of drugs on patients suffering from schizophrenia and other disorders."
ITI-007 rapidly penetrates the brain after oral administration and interacts with molecular targets important in a variety of central nervous system disorders. Taken together, these data suggest that ITI-007 exhibits a unique and beneficial pharmacological profile useful for the treatment of schizophrenia, mood disorders and insomnia.
SOURCE Intra-Cellular Therapies, Inc.